Intelence- New drug for patients with HIV-1 infection

Product:

Intelence

Company:

Tibotec

Pharmacologic class:

Antiretroviral (non-nucleoside reverse transcriptase inhibitor)

Active ingredient:

Etravirine 100 mg; tabs.

Indication:

HIV-1 infection, in combination with other antiretrovirals, in
treatment-experienced adults with evidence of viral replication and HIV-1 strains resistant to a non-nucleoside reverse transcriptase inhibitor (NNRTI) and other antiretrovirals.

Pharmacology:

Etravirine is an NNRTI. It works by blocking RNA-dependent and DNA-dependent DNA polymerase activity of HIV-1.

After oral administration, maximum plasma levels are reached in about 2.5-4 hours. For maximum absorption, etravirine should be taken after a meal. It is highly protein-bound, primarily to albumin and alpha 1-acid glycoprotein, and metabolized by the liver to mostly inactive metabolites. Mild-to-moderate hepatic impairment does not affect its metabolism, but patients with severe hepatic impairment have not been studied.

Clinical trials:

The approval for this drug was based on analyses of two randomized, double-blind, placebo-controlled studies that were conducted in clinically advanced, three-class antiretroviral treatment-experienced adults. These studies compared etravirine + background regimen with placebo + background regimen. All subjects received darunavir/ritonavir as part of their background regimen and at least two other investigator-selected antiretrovirals.

Subjects were treatment-
experienced HIV-1 infected patients with plasma HIV-1 RNA levels of >5,000 copies/mL while on a stable antiretroviral regimen for at least eight weeks; they had at least one NNRTI resistance-associated mutation and three or more specific protease inhibitor (PI) mutations. Virologic response was defined as an undetectable viral load (<50 copies/mL of viral RNA) at 24 weeks. Pooled results for the two studies indicated that, at 24 weeks, 59.8% of the patients given etravirine + background regimen were responders, compared with 40.2% for the placebo group. At week 24, 74% of the etravirine-treated group had a viral load of <400 copies/mL, compared with 51.5% of the placebo group. Studies are continuing.

Adults:

Take after meals. May disperse tabs in water and drink. 200 mg twice daily.

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